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Cephalosporins
IDIT Walters
18
Pharmacology
02/05/2011

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Term
Cephalosporins
Definition

Starts w/ Cepha- or Cefa-

 

StructureB-lactam + dihydrothiazine ring + side chain

 

Mechanism:  Inhibits transpeptidase (same as PCN)

Advantage over PCNs: resist many B-lactamases

Term
Cefazolin
Definition

1st gen Cephalosporin

Resist Staph PCNase

 

G+, and G- (PEcK - Proteus, E. coli, Kleibsiella)
PEcK INC urinary pH --> urinary stones

 

 

IV

Term
Cephalexin
Definition

1st gen Cephalosporin

Resist Staph PCNase

 

G+, and G- (PEcK - Proteus, E. coli, Kleibsiella)
PEcK INC urinary pH --> urinary stones

 

Oral

Term
Cefadroxil
Definition

1st gen Cephalosporin

Resist Staph PCNase

 

G+, and G- (PEcK - Proteus, E. coli, Kleibsiella)
PEcK INC urinary pH --> urinary stones

Oral

Term
Cefaclor
Definition

2nd gen Cephalosporins

Less G+, INC G -

Covers PEcK + H. influenza & some Neisseria (HNPEcK)

 

Oral every 8 hrs, assoc w/ serum sickness Sx

Term
Cefuroxime
Definition

2nd gen Cephalosporins

Less G+, INC G -

Covers PEcK + H. influenza & some Neisseria (HNPEcK)

 

q 12 hr

Oral, IV, IM

Term
Cefoxitin
Definition

2nd gen Cephalosporins

Less G+, INC G -

Covers PEcK + H. influenza & some Neisseria (HNPEcK)

 

Cephamycin

 

Use:  Bacteroides fragilis

Term
Cefotetan
Definition

2nd gen Cephalosporins

Less G+, INC G -

Covers PEcK + H. influenza & some Neisseria (HNPEcK)

 

MTT (methylthiotetrazole) side-chain antagonizes Vit K --> hypoprothrombinemia; must supp w/Vit K

 

**Dosage depends on pt compliance

Term
Ceftriaxone
Definition

3rd gen Cephalosporin

Less G +, INC G -

 

IV/IM

 

Highly protein bound, displaces bilirubin, Caution: do not use <3 mo old, unless single dose for gonorrhoeae conjunctivitis

 

1/2 excreted in urine, 1/2 in bile

 

UsesMeningtitis (fr S. penumonieae & N. meningitidis)

 

FDA:  Do not use w/ Ca products in pts <28 days old; older pts - give Rx sequentially, flush line, wait 48 hrs in bet Rx and Ca product

 

SIDE EFFECTS'sludge' in kids (nausea, anorexia, etc), reversible, hepatitis (rare)

Term
Cefotaxime
Definition

3rd gen Cephalosporin

Less G +, INC G -, Bacteroides

IV/IM

Parent & metabolic active

Term
Cefpodoxime
Definition

3rd gen Cephalosporin

Less G +, INC G -

Oral

Term
Cefdinir
Definition

3rd gen Cephalosporin

Less G +, INC G - 

 

Oral 

 

Excreted unchanged

 

Binds Fe --> DEC absorption; reddens feces in infants on formula (high in Fe)

Term
Ceftazidime
Definition

3rd gen Cephalosporin

Less G +, INC G -

IV/IM

Side Effectsneuorologic (myoclonus, EEG changes, disorientation), Caution if epiletic

Term
Cefepime
Definition

4th gen Cephalosporin

 

Use:  G- rods resistant to 3rd gen

 

IV/IM

 

Side Effectsneurologic (disorientation, myoclonus, EEG changes), Caution if epiletic

 

Renal excretion - adjust for renal function

Term
Cefditoren
Definition

4th gen Cephalosporin

 

G- rods resistant to 3rd gen

 

Pro-drug (must be activated)

Hydrolyzed by esterases

Term
Ceftaroline
Definition

Advanced gen

 

IV proRx q 12 hr for CABP (community-acquired bacterial pneumonia), skin infections (MRSA)

 

Side Effectsnausea, diarrhea, rash

Term
General Side Effects of ALL Cephalosporins
Definition
  • Hypersensitivity - risk of cross-allergy w/PCN > w/1st gen unless documented Type I IgE to PCN
  • Nephrotoxicity - but lower than aminoglycosides
  • FDA: risk of immune-mediated hemolytic anemia
Term
Carbapenems
Definition

Ends in -penim

 

Broadest B-lactams

 

G + / -, anaerobes, resistant infections

 

Rx. Interaction (class effect) - DEC valproic acid --> INC seizures

  • Impenim w/Cilastatin - IV/IM - UTIs

 

Cilastatin - dehydropeptidase inhibitor

Side Effects:  N&V, seizures (1.5%)

  • Meropenem - fewer seizers (0.5%)

  • Ertapenem

  • Doripenem

  •